1400W 2HCl

別名: N-(3-(Aminomethyl)benzyl)acetamidine 中文名稱：N-[3-(氨甲基)芐基]乙脒二鹽酸鹽

目錄號(hào)：S8337 Purity: 99.89%

1400W (N-(3-(Aminomethyl)benzyl)acetamidine) 是iNOS的抑制劑，與iNOS緩慢、緊密地結(jié)合，具有選擇性。

1400W 2HCl Chemical Structure

CAS: 214358-33-5

規(guī)格	價(jià)格	庫(kù)存
10mM (1mL in DMSO)	1040.13	現(xiàn)貨
10mg	794.67	現(xiàn)貨
50mg	3251.58	現(xiàn)貨
200mg	8166.25	現(xiàn)貨
1g	24489.05	現(xiàn)貨
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產(chǎn)品質(zhì)控

批次：純度： 99.89%

99.89

1400W 2HCl相關(guān)產(chǎn)品

相關(guān)靶點(diǎn)	nNOS eNOS iNOS	點(diǎn)擊展開
相關(guān)產(chǎn)品	L-NAME HCl Falcarindiol L-NMMA acetate TPEN 2',5'-Dihydroxyacetophenone	點(diǎn)擊展開
相關(guān)化合物庫(kù)	激酶抑制劑庫(kù) FDA藥物庫(kù) 天然產(chǎn)物庫(kù) 已知活性藥物庫(kù)-I 生物活性庫(kù)Ⅱ	點(diǎn)擊展開

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類型	給藥濃度	孵育時(shí)間	活性描述	文獻(xiàn)信息
RAW264.7	Antiinflammatory assay	50 uM	24 hrs	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitrite production at 50 uM treated 30 mins before LPS challenge measured after 24 hrs by Griess method	20447741
RAW264.7	Antiinflammatory assay	0.5 to 2 uM	2 hrs	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced COX-2 expression at 0.5 to 2 uM incubated for 2 hrs prior to LPS challenge measured after 24 hrs by Western blot analysis	23232148
RAW264.7	Antiinflammatory assay	2 uM	2 hrs	Antiinflammatory activity in mouse RAW264.7 cells assessed as downregulation of LPS-induced iNOS mRNA expression at 2 uM incubated for 2 hrs prior to LPS challenge measured after 9 hrs by RT-PCR analysis	23232148
RAW264.7	Antiinflammatory assay	0.5 to 2 uM	2 hrs	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced iNOS expression at 0.5 to 2 uM incubated for 2 hrs prior to LPS challenge measured after 24 hrs by Western blot analysis	23232148
RAW264.7	Function assay	4 uM		Inhibition iNOS mRNA expression levels in LPS-induced mouse RAW264.7 cells at 4 uM by RT-PCR analysis	27542306
RAW264.7	Function assay	4 uM		Inhibition iNOS protein expression levels in LPS-induced mouse RAW264.7 cells at 4 uM by Western blot analysis	27542306
RAW264.7	Antiinflammatory assay		24 hrs	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay, IC50=0.2μM	23232148
RAW264.7	Antiinflammatory assay		20 hrs	Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as nitrite accumulation after 20 hrs by fluorimetry, IC50=0.3μM	11678654
RAW264.7	Antiinflammatory assay		24 hrs	Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced nitrite accumulation after 24 hrs, IC50=2.9μM	15568764
RAW264.7	Antiinflammatory assay		24 hrs	Antiinflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as effect on NO production pretreated 1 hr before LPS challenge measured after 24 hrs, IC50=3.1μM	11908984
RAW 264	Function assay		24 hrs	Inhibition of 1ug/ml LPS-stimulated nitirc oxide accumulation in RAW 264 cells after 24 hrs, IC50=5.2μM	17320246
N9	Antiinflammatory assay		24 hrs	Antiinflammatory activity against mouse N9 cells assessed as inhibition of LPS/IFN-gamma-induced nitrite accumulation after 24 hrs, IC50=6.3μM	15568764
RAW264.7	Cytotoxicity assay		24 hrs	Cytotoxicity against mouse RAW264.7 cells assessed as cell viability after 24 hrs by MTS assay, IC50=47.47μM	23232148
RAW264.7	Function assay			Inhibition of LPS-induced nitric oxide generation in mouse RAW264.7 cells pretreated 1 hr before LPS challenge by Griess method, IC50=1.5μM	19278854
N9	Function assay			Inhibitory effect of compound on the accumulation of NO2 in the culture media of N9 cells in response to LPS/IFN-gamma, IC50=2.2μM	15013012
RAW264.7	Antiinflammatory assay			Antiinflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of nitric oxide production pretreated 1 hr before LPS challenge, IC50=2.3μM	12662101
RAW264.7	Function assay			Inhibition of LPS-induced nitric oxide accumulation in mouse RAW264.7 cells, IC50=2.7μM	19699097
N9	Antiinflammatory assay			Antiinflammatory activity in LPS/IFN-gamma-stimulated mouse N9 cells assessed as inhibition of nitric oxide production pretreated 1 hr before LPS/IFNgamma challenge, IC50=3.6μM	12662101
RAW264.7	Function assay			Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells, IC50=3.78μM	17988874
RAW264.7	Function assay			Inhibitory effect of compound on the accumulation of NO2 in the culture media of RAW 264.7 cells in response to LPS, IC50=6.1μM	15013012
點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

1400W (N-(3-(Aminomethyl)benzyl)acetamidine) 是iNOS的抑制劑，與iNOS緩慢、緊密地結(jié)合，具有選擇性。

靶點(diǎn)

iNOS ^[1] (Cell-free assay)	nNOS ^[1] (Cell-free assay)	eNOS ^[1] (Cell-free assay)
<7 nM(Kd)	2 μM(Ki)	50 μM(Ki)

體外研究(In Vitro)
體外研究活性	1400W是一種不可逆的抑制劑或是一種具有積極緩慢的可逆性的抑制劑，抑制iNOS。1400對(duì)于人源iNOS的抑制作用是時(shí)間依賴性的。1400W與L-arginine屬于競(jìng)爭(zhēng)關(guān)系，不是iNOS的底物^[1]。
細(xì)胞實(shí)驗(yàn)	細(xì)胞系	RAW264.7細(xì)胞
	濃度	100 μM
	孵育時(shí)間	16 h
	方法	用LPS/IFNγ和iNOS的抑制劑1400W（100 μM）處理RAW264.7，處理16小時(shí)。GAPDH-P300的結(jié)合被1400W抑制。獲取細(xì)胞裂解液，用anti-p300的抗體進(jìn)行免疫沉淀，免疫沉淀物用于WB分析。

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	1400W在大鼠中選擇性地抑制微脈管系統(tǒng)損傷。在大鼠內(nèi)毒素誘導(dǎo)的血管損傷模型中，1400W對(duì)iNOS的抑制作用比eNOS有效50倍以上。除此之外，1400W還在結(jié)腸、肝臟、腎臟和心臟處濃度依賴性地減少LPS誘導(dǎo)的、與iNOS誘導(dǎo)相關(guān)的血管滲漏.對(duì)于除去腎臟的其他器官，其保護(hù)作用幾近100%，而在腎臟中式54%^[1]。1400W在腎臟缺血再灌注的大鼠模型中，對(duì)腎臟的氧化和硝化壓力具有改善作用^[2]。在小鼠中，處理以1400W可以減少實(shí)體瘤的生長(zhǎng)速率^[4]。
動(dòng)物實(shí)驗(yàn)	Animal Models	大鼠
	Dosages	0.1-10 mg/kg
	Administration	皮下注射

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗(yàn)信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT00845169	Completed	Endothelial Dysfunction	University of Edinburgh\|NHS Lothian\|Ume? University	April 2012	Not Applicable

參考文獻(xiàn)
[1] Garvey EP, et al. J Biol Chem. 199, 272(8):4959-63. [2] Ersoz N, et al. Ren Fail. 2009, 31(8):704-10. [3] Sen N, et al. Nat Cell Biol. 2008, 10(7):866-73. [4] Thomsen LL, et al. Cancer Res. 1997, 57(15):3300-4. + 展開

參考文獻(xiàn)

[1] Garvey EP, et al. J Biol Chem. 199, 272(8):4959-63.
[2] Ersoz N, et al. Ren Fail. 2009, 31(8):704-10.
[3] Sen N, et al. Nat Cell Biol. 2008, 10(7):866-73.

[4] Thomsen LL, et al. Cancer Res. 1997, 57(15):3300-4.

+ 展開

化學(xué)信息&溶解度

分子量	250.17	分子式	C₁₀H₁₅N₃.2HCl
CAS號(hào)	214358-33-5	SDF	Download 1400W 2HCl SDF
Smiles	CC(=NCC1=CC=CC(=C1)CN)N.Cl.Cl
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1個(gè)月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 35 mg/mL ( (139.9 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Water : 35 mg/mL (139.9 mM)

Ethanol : 35 mg/mL (139.9 mM)

DMSO : 50 mg/mL ( (199.86 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Water : 50 mg/mL (199.86 mM)

Ethanol : 13 mg/mL (51.96 mM)

DMSO : 50 mg/mL ( (199.86 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Water : 50 mg/mL (199.86 mM)

Ethanol : 12 mg/mL (47.96 mM)

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計(jì)算器分子量計(jì)算器

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過(guò)程中的損耗，建議多配一只動(dòng)物的藥量）

給藥劑量 mg/kg 動(dòng)物平均體重 g 每只動(dòng)物給藥體積 μL 動(dòng)物數(shù)量只

第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過(guò)該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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